BRENDA - Enzyme Database show

Gemcitabine uptake in glioblastoma multiforme: potential as a radiosensitizer

Sigmond, J.; Honeywell, R.J.; Postma, T.J.; Dirven, C.M.; de Lange, S.M.; van der Born, K.; Laan, A.C.; Baayen, J.C.; Van Groeningen, C.J.; Bergman, A.M.; Giaccone, G.; Peters, G.J.; Ann. Oncol. 20, 182-187 (2009)

Data extracted from this reference:

Application
EC Number
Application
Commentary
Organism
3.5.4.5
medicine
studies on radiosensitization of glioblastoma multiforme (GBM), deoxynucleoside analogue gemcitabine (dFdC) considered for combination therapy with radiation in glioblastomas
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
3.5.4.5
0.0092
-
2',2'-difluorodeoxycytidine
i.e. gemcitabine, variation of plasma gemcitabine between 0.9 and 9.2 microM
Homo sapiens
3.5.4.5
0.0726
-
2',2'-difluorodeoxyuridine
i.e. dFdU, variation of plasma ranges between 24.9 and 72.6 microM
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.5.4.5
deoxycytidine + H2O
Homo sapiens
-
deoxyuridine + NH3
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
3.5.4.5
Homo sapiens
-
glioblastoma multiforme (GBM) patients
-
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
3.5.4.5
blood plasma
glioblastoma multiforme (GBM) patients
Homo sapiens
-
3.5.4.5
glioblastoma multiforme cell
glioblastoma multiforme (GBM) patients
Homo sapiens
-
Specific Activity [micromol/min/mg]
EC Number
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
3.5.4.5
additional information
-
variation between 1.51 to 5.50 nmol/h/mg protein, about 100-fold lower than that in liver
Homo sapiens
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.4.5
2',2'-difluorodeoxycytidine + H2O
deamination of the deoxynucleoside analogue gemcitabine (dFdC) to difluorodeoxyuridine (dFdU), difluorodeoxyuridine used as radiosensitizer in gene therapy
695606
Homo sapiens
2',2'-difluorodeoxyuridine + NH3
-
-
-
?
3.5.4.5
deoxycytidine + H2O
-
695606
Homo sapiens
deoxyuridine + NH3
-
-
-
?
Temperature Optimum [°C]
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
3.5.4.5
37
-
assay at
Homo sapiens
Application (protein specific)
EC Number
Application
Commentary
Organism
3.5.4.5
medicine
studies on radiosensitization of glioblastoma multiforme (GBM), deoxynucleoside analogue gemcitabine (dFdC) considered for combination therapy with radiation in glioblastomas
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
3.5.4.5
0.0092
-
2',2'-difluorodeoxycytidine
i.e. gemcitabine, variation of plasma gemcitabine between 0.9 and 9.2 microM
Homo sapiens
3.5.4.5
0.0726
-
2',2'-difluorodeoxyuridine
i.e. dFdU, variation of plasma ranges between 24.9 and 72.6 microM
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.5.4.5
deoxycytidine + H2O
Homo sapiens
-
deoxyuridine + NH3
-
-
?
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
3.5.4.5
blood plasma
glioblastoma multiforme (GBM) patients
Homo sapiens
-
3.5.4.5
glioblastoma multiforme cell
glioblastoma multiforme (GBM) patients
Homo sapiens
-
Specific Activity [micromol/min/mg] (protein specific)
EC Number
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
3.5.4.5
additional information
-
variation between 1.51 to 5.50 nmol/h/mg protein, about 100-fold lower than that in liver
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.4.5
2',2'-difluorodeoxycytidine + H2O
deamination of the deoxynucleoside analogue gemcitabine (dFdC) to difluorodeoxyuridine (dFdU), difluorodeoxyuridine used as radiosensitizer in gene therapy
695606
Homo sapiens
2',2'-difluorodeoxyuridine + NH3
-
-
-
?
3.5.4.5
deoxycytidine + H2O
-
695606
Homo sapiens
deoxyuridine + NH3
-
-
-
?
Temperature Optimum [°C] (protein specific)
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
3.5.4.5
37
-
assay at
Homo sapiens